Alginate/chitosan microparticles for tamoxifen delivery to the lymphatic system.
Oral administration of the nonsteroidal anti-estrogen tamoxifen (TMX) is the treatment of choice for metastatic estrogen receptor-positive breast cancer. With the aim to improve TMX oral bioavailability and decrease its side effects, crosslinked alginate microparticles for the targeting to the lymphatic system by Peyer's patch (PP) uptake were developed and in vitro characterized. TMX was molecularly dispersed inside the microparticles and an electrostatic interaction involving the TMX tertiary amine was detected by rheological and FT-IR assays. Microparticles showed a size less than 3mum, then suitability to be taken up by M cells in PP and a positive surface charge. Moreover, TMX loading level as well as in vitro release behaviour was affected by the polymer network connected with the mannuronic/guluronic ratio of the alginate chains.
Coppi
G
G
Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Via Campi 183, 41100 Modena, Italy. gilberto.coppi@unimore.it
Iannuccelli
V
V
D000464:Alginates / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D048271:Chitosan / Q000737:chemistry*; D003432:Cross-Linking Reagents / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding; D004965:Estrogen Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D010581:Peyer's Patches / Q000378:metabolism*; D012212:Rheology; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013499:Surface Properties; D013629:Tamoxifen / Q000008:administration & dosage* / Q000493:pharmacokinetics
D000464:Alginates; D003432:Cross-Linking Reagents; D004337:Drug Carriers; D004965:Estrogen Antagonists; D006603:Hexuronic Acids; D013629:Tamoxifen; D020723:Glucuronic Acid; D048271:Chitosan